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  1. Article ; Online: Investigation of the structure-activity relationship in ponericin L1 from

    Senetra, Alexandria S / Necelis, Matthew R / Caputo, Gregory A

    Peptide science (Hoboken, N.J.)

    2020  Volume 112, Issue 3

    Abstract: Naturally derived antimicrobial peptides have been an area of great interest because of high selectivity against bacterial targets over host cells and the limited development of bacterial resistance to these molecules throughout evolution. There are also ...

    Abstract Naturally derived antimicrobial peptides have been an area of great interest because of high selectivity against bacterial targets over host cells and the limited development of bacterial resistance to these molecules throughout evolution. There are also a significant number of venom-derived peptides that exhibit antimicrobial activity in addition to activity against mammals or other organisms. Many venom peptides share the same net cationic, amphiphilic nature as host-defense peptides, making them an attractive target for development as potential antibacterial agents. The peptide ponericin L1 derived from
    Language English
    Publishing date 2020-03-31
    Publishing country United States
    Document type Journal Article
    ISSN 2475-8817
    ISSN (online) 2475-8817
    DOI 10.1002/pep2.24162
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article: Pharmacokinetic Interaction of Kratom and Cannabidiol in Male Rats.

    Berthold, Erin C / Kamble, Shyam H / Kanumuri, Siva Rama Raju / Kuntz, Michelle A / Senetra, Alexandria S / Chiang, Yi-Hua / Mukhopadhyay, Sushobhan / McCurdy, Christopher R / Sharma, Abhisheak

    Pharmaceutics

    2024  Volume 16, Issue 3

    Abstract: Kratom and cannabidiol products are used to self-treat a variety of conditions, including anxiety and pain, and to elevate mood. Research into the individual pharmacokinetic properties of commercially available kratom and cannabidiol products has been ... ...

    Abstract Kratom and cannabidiol products are used to self-treat a variety of conditions, including anxiety and pain, and to elevate mood. Research into the individual pharmacokinetic properties of commercially available kratom and cannabidiol products has been performed, but there are no studies on coadministration of these products. Surveys of individuals with kratom use history indicate that cannabidiol use is one of the strongest predictors of both lifetime and past month kratom use. The purpose of this study was to determine if there are changes in pharmacokinetic properties when commercially available kratom and cannabidiol products are administered concomitantly. It was found that with concomitant administration of cannabidiol, there was a 2.8-fold increase in the exposure of the most abundant kratom alkaloid, mitragynine, and increases in the exposure of other minor alkaloids. The results of this work suggest that with cannabidiol coadministration, the effects of kratom may be both delayed and increased due to a delay in time to reach maximum plasma concentration and higher systemic exposure of the psychoactive alkaloids found in kratom.
    Language English
    Publishing date 2024-02-24
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2527217-2
    ISSN 1999-4923
    ISSN 1999-4923
    DOI 10.3390/pharmaceutics16030318
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  3. Article ; Online: Preclinical pharmacokinetic studies of villocarine A, an active Uncaria alkaloid.

    Chiang, Yi-Hua / Chear, Nelson Jeng-Yeou / Berthold, Erin C / Kuntz, Michelle A / Kanumuri, Siva Rama Raju / Senetra, Alexandria S / Ramanathan, Surash / McCurdy, Christopher R / Sharma, Abhisheak

    Drug testing and analysis

    2024  

    Abstract: Villocarine A is a bioactive indole alkaloid isolated from the Uncaria genus. It has demonstrated vasorelaxation activity and potential to protect the central nervous system. To identify the pharmacokinetic properties of villocarine A, a series of in ... ...

    Abstract Villocarine A is a bioactive indole alkaloid isolated from the Uncaria genus. It has demonstrated vasorelaxation activity and potential to protect the central nervous system. To identify the pharmacokinetic properties of villocarine A, a series of in vitro and in vivo studies have been performed. Villocarine A was found to be highly permeable (15.6 ± 1.6*10
    Language English
    Publishing date 2024-05-15
    Publishing country England
    Document type Journal Article
    ZDB-ID 2462336-2
    ISSN 1942-7611 ; 1942-7603
    ISSN (online) 1942-7611
    ISSN 1942-7603
    DOI 10.1002/dta.3703
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  4. Article: Pharmacokinetics of delta-9-tetrahydrocannabinol following acute cannabis smoke exposure in mice; effects of sex, age, and strain.

    Gazarov, Emely A / Zequeira, Sabrina / Senetra, Alexandria S / Howard, John / Sharma, Abhisheak / McCurdy, Christopher R / Lewis, Jada / Bizon, Jennifer L / Setlow, Barry

    Frontiers in pharmacology

    2023  Volume 14, Page(s) 1227220

    Abstract: Increased use of cannabis and cannabinoids for recreational and medical purposes has led to a growth in research on their effects in animal models. The majority of this work has employed cannabinoid injections; however, smoking remains the most common ... ...

    Abstract Increased use of cannabis and cannabinoids for recreational and medical purposes has led to a growth in research on their effects in animal models. The majority of this work has employed cannabinoid injections; however, smoking remains the most common route of cannabis consumption. To better model real-world cannabis use, we exposed mice to cannabis smoke to establish the pharmacokinetics of Δ9THC and its metabolites in plasma and brain. To determine the time course of Δ9THC and two major metabolites [11-hydroxy-delta-9-tetrahydrocannabinol (11-OH-THC) and 11-nor-9-carboxy-delta-9-tetrahydrocannabinol (11-COOH-THC)], male and female C57BL/6J mice were exposed to smoke from sequentially burning 5 cannabis cigarettes. Following smoke exposure, trunk blood and brains were collected at 6 time points (10-240 min). Plasma and brain homogenates were analyzed for Δ9THC and metabolites using a validated ultraperformance liquid chromatography-tandem mass spectrometry method. To assess effects of age, sex, and mouse strain, we exposed mice of four strains (C57BL/6J, FVB, Swiss Webster, and 129S6/SvEv, aged 4-24 months) to cannabis using the same smoke regimen. Samples were collected 10 and 40 min following exposure. Lastly, to assess effects of dose, C57BL/6J mice were exposed to smoke from burning 3 or 5 cannabis cigarettes, with samples collected 40 min following exposure. The pharmacokinetic study revealed that maximum plasma Δ9THC concentrations (C
    Language English
    Publishing date 2023-08-28
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2587355-6
    ISSN 1663-9812
    ISSN 1663-9812
    DOI 10.3389/fphar.2023.1227220
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  5. Article ; Online: Comparative Pharmacokinetics of Commercially Available Cannabidiol Isolate, Broad-Spectrum, and Full-Spectrum Products.

    Berthold, Erin C / Kamble, Shyam H / Kanumuri, Siva Rama Raju / Kuntz, Michelle A / Senetra, Alexandria S / Chiang, Yi-Hua / McMahon, Lance R / McCurdy, Christopher R / Sharma, Abhisheak

    European journal of drug metabolism and pharmacokinetics

    2023  Volume 48, Issue 4, Page(s) 427–435

    Abstract: Background and objectives: A wide variety of products containing cannabidiol (CBD) are available on the commercial market. One of the most common products, CBD oil, is administered to self-treat a variety of conditions. These oils are available as CBD ... ...

    Abstract Background and objectives: A wide variety of products containing cannabidiol (CBD) are available on the commercial market. One of the most common products, CBD oil, is administered to self-treat a variety of conditions. These oils are available as CBD isolate, broad-spectrum [all terpenes and minor cannabinoids except Δ-9-tetrahydrocannabinol (THC)], or full-spectrum (all terpenes and minor cannabinoids with THC < 0.3% dried weight) products. A systematic pharmacokinetic study was performed to determine whether there are differences in the pharmacokinetic parameters and systemic exposure of CBD after oral dosing as an isolate, broad-spectrum, or full-spectrum product.
    Methods: Male and female Sprague Dawley rats were treated with a single, equivalent oral dose of CBD delivered as isolate, broad-spectrum, or full-spectrum product. An additional study using an in-house preparation of CBD isolate plus 0.2% THC was performed. A permeability assay was also conducted to investigate whether the presence of THC alters the intestinal permeability of CBD.
    Results: There was an increase in the oral bioavailability of CBD (12% and 21% in male and female rats, respectively) when administered as a full-spectrum product compared with the isolate and broad-spectrum products. There was no difference in the bioavailability of CBD between the commercially available full-spectrum formulation (3.1% CBD; containing 0.2% THC plus terpenes and other minor cannabinoids) versus the in-house preparation of CBD full-spectrum (CBD isolate 3.2% plus 0.2% THC isolate). In vitro permeability assays demonstrated that the presence of THC increases permeability of CBD while also decreasing efflux through the gut wall.
    Conclusions: The presence of 0.2% THC increased the oral bioavailability of CBD in male and female rats, indicating that full-spectrum products may produce increased effectiveness of CBD due to a greater exposure available systemically.
    MeSH term(s) Male ; Female ; Rats ; Animals ; Cannabidiol ; Dronabinol ; Rats, Sprague-Dawley ; Cannabinoids ; Biological Availability
    Chemical Substances Cannabidiol (19GBJ60SN5) ; Dronabinol (7J8897W37S) ; Cannabinoids
    Language English
    Publishing date 2023-06-19
    Publishing country France
    Document type Journal Article
    ZDB-ID 196729-0
    ISSN 2107-0180 ; 0398-7639 ; 0378-7966
    ISSN (online) 2107-0180
    ISSN 0398-7639 ; 0378-7966
    DOI 10.1007/s13318-023-00839-3
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  6. Article ; Online: FABP5 is important for cognitive function and is an important regulator of the physiological effects and pharmacokinetics of acute Δ9 tetrahydrocannabinol inhalation in mice.

    Penman, Samantha L / Roeder, Nicole M / Berthold, Erin C / Senetra, Alexandria S / Marion, Matthew / Richardson, Brittany J / White, Olivia / Fearby, Nathan L / McCurdy, Christopher R / Hamilton, John / Sharma, Abhisheak / Thanos, Panayotis K

    Pharmacology, biochemistry, and behavior

    2023  Volume 231, Page(s) 173633

    Abstract: Fatty acid binding protein 5 (FABP5) interacts with the endocannabinoid system in the brain via intracellular transport of anandamide, as well as Δ9-tetrahydrocannabinol (THC), the main psychoactive component of cannabis. Previous work has established ... ...

    Abstract Fatty acid binding protein 5 (FABP5) interacts with the endocannabinoid system in the brain via intracellular transport of anandamide, as well as Δ9-tetrahydrocannabinol (THC), the main psychoactive component of cannabis. Previous work has established the behavioral effects of genetic deletion of FABP5, but not in the presence of THC. The present study sought to further elucidate the role of FABP5 on the pharmacokinetic and behavioral response to THC through global deletion. Adult FABP5
    MeSH term(s) Animals ; Mice ; Brain/metabolism ; Chromatography, Liquid ; Cognition ; Dronabinol/pharmacology ; Fatty Acid-Binding Proteins/genetics ; Fatty Acid-Binding Proteins/metabolism ; Fatty Acid-Binding Proteins/pharmacology ; Tandem Mass Spectrometry
    Chemical Substances Dronabinol (7J8897W37S) ; Fatty Acid-Binding Proteins ; Fabp5 protein, mouse
    Language English
    Publishing date 2023-09-15
    Publishing country United States
    Document type Journal Article ; Research Support, N.I.H., Extramural ; Research Support, Non-U.S. Gov't
    ZDB-ID 191042-5
    ISSN 1873-5177 ; 0091-3057
    ISSN (online) 1873-5177
    ISSN 0091-3057
    DOI 10.1016/j.pbb.2023.173633
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  7. Article ; Online: Synergistic interactions of ionic liquids and antimicrobials improve drug efficacy.

    Yang, Daniel D / Paterna, Nicholas J / Senetra, Alexandria S / Casey, Kaitlyn R / Trieu, Phillip D / Caputo, Gregory A / Vaden, Timothy D / Carone, Benjamin R

    iScience

    2020  Volume 24, Issue 1, Page(s) 101853

    Abstract: Combinations of ionic liquids (ILs) with antimicrobial compounds have been shown to produce synergistic activities in model liposomes. In this study, imidazolium chloride-based ILs with alkyl tail length variations are combined with commercially ... ...

    Abstract Combinations of ionic liquids (ILs) with antimicrobial compounds have been shown to produce synergistic activities in model liposomes. In this study, imidazolium chloride-based ILs with alkyl tail length variations are combined with commercially available, small-molecule antimicrobials to examine the potential for combinatorial and synergistic antimicrobial effects on
    Language English
    Publishing date 2020-11-23
    Publishing country United States
    Document type Journal Article
    ISSN 2589-0042
    ISSN (online) 2589-0042
    DOI 10.1016/j.isci.2020.101853
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  8. Article ; Online: Correlating Lipid Membrane Permeabilities of Imidazolium Ionic Liquids with their Cytotoxicities on Yeast, Bacterial, and Mammalian Cells.

    Cook, Kendall / Tarnawsky, Katharine / Swinton, Alana J / Yang, Daniel D / Senetra, Alexandria S / Caputo, Gregory A / Carone, Benjamin R / Vaden, Timothy D

    Biomolecules

    2019  Volume 9, Issue 6

    Abstract: Alkyl-imidazolium chloride ionic liquids (ILs) have been broadly studied for biochemical and biomedical technologies. They can permeabilize lipid bilayer membranes and have cytotoxic effects, which makes them targets for drug delivery biomaterials. We ... ...

    Abstract Alkyl-imidazolium chloride ionic liquids (ILs) have been broadly studied for biochemical and biomedical technologies. They can permeabilize lipid bilayer membranes and have cytotoxic effects, which makes them targets for drug delivery biomaterials. We assessed the lipid-membrane permeabilities of ILs with increasing alkyl chain lengths from ethyl to octyl groups on large unilamellar vesicles using a trapped-fluorophore fluorescence lifetime-based leakage experiment. Only the most hydrophobic IL, with the octyl chain, permeabilizes vesicles, and the concentration required for permeabilization corresponds to its critical micelle concentration. To correlate the model vesicle studies with biological cells, we quantified the IL permeabilities and cytotoxicities on different cell lines including bacterial, yeast, and ovine blood cells. The IL permeabilities on vesicles strongly correlate with permeabilities and minimum inhibitory concentrations on biological cells. Despite exhibiting a broad range of lipid compositions, the ILs appear to have similar effects on the vesicles and cell membranes.
    MeSH term(s) Animals ; Anti-Infective Agents/chemistry ; Anti-Infective Agents/metabolism ; Anti-Infective Agents/pharmacology ; Anti-Infective Agents/toxicity ; Bacteria/drug effects ; Bacteria/metabolism ; Cell Membrane Permeability ; Erythrocytes/drug effects ; Erythrocytes/metabolism ; Hydrophobic and Hydrophilic Interactions ; Imidazoles/chemistry ; Imidazoles/metabolism ; Imidazoles/pharmacology ; Imidazoles/toxicity ; Ionic Liquids/chemistry ; Ionic Liquids/metabolism ; Ionic Liquids/pharmacology ; Ionic Liquids/toxicity ; Saccharomyces cerevisiae/drug effects ; Saccharomyces cerevisiae/metabolism ; Sheep
    Chemical Substances Anti-Infective Agents ; Imidazoles ; Ionic Liquids ; imidazole (7GBN705NH1)
    Language English
    Publishing date 2019-06-25
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2701262-1
    ISSN 2218-273X ; 2218-273X
    ISSN (online) 2218-273X
    ISSN 2218-273X
    DOI 10.3390/biom9060251
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  9. Article ; Online: The Lack of Contribution of 7-Hydroxymitragynine to the Antinociceptive Effects of Mitragynine in Mice: A Pharmacokinetic and Pharmacodynamic Study.

    Berthold, Erin C / Kamble, Shyam H / Raju, Kanumuri S / Kuntz, Michelle A / Senetra, Alexandria S / Mottinelli, Marco / León, Francisco / Restrepo, Luis F / Patel, Avi / Ho, Nicholas P / Hiranita, Takato / Sharma, Abhisheak / McMahon, Lance R / McCurdy, Christopher R

    Drug metabolism and disposition: the biological fate of chemicals

    2021  Volume 50, Issue 2, Page(s) 158–167

    Abstract: Kratom ( ...

    Abstract Kratom (
    MeSH term(s) Analgesics, Opioid/pharmacology ; Animals ; Female ; Male ; Mice ; Mice, Inbred C57BL ; Secologanin Tryptamine Alkaloids/pharmacology
    Chemical Substances Analgesics, Opioid ; Secologanin Tryptamine Alkaloids ; 7-hydroxymitragynine (2T3TWA75R0) ; mitragynine (EP479K822J)
    Language English
    Publishing date 2021-11-10
    Publishing country United States
    Document type Journal Article ; Research Support, N.I.H., Extramural ; Research Support, Non-U.S. Gov't
    ZDB-ID 186795-7
    ISSN 1521-009X ; 0090-9556
    ISSN (online) 1521-009X
    ISSN 0090-9556
    DOI 10.1124/dmd.121.000640
    Database MEDical Literature Analysis and Retrieval System OnLINE

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